Assay Detail
Binding
CHEMBL644296
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity measured against rat lens aldose reductase using 3-pyridinecarboxaldehyde as substrate
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Aldo-keto reductase family 1 member B1 (CHEMBL2622) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.81 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL436 | TOLRESTAT | 4.0 | 1 | 8.54 |
| CHEMBL56337 | EPALRESTAT | 4.0 | 1 | 7.89 |
| CHEMBL7679 | PONALRESTAT | 2.0 | 1 | 7.55 |
| CHEMBL269550 | — | — | 1 | 7.33 |
| CHEMBL266497 | SORBINIL | 3.0 | 1 | 6.55 |
| CHEMBL7480 | ALCONIL | — | 1 | 6.52 |
| CHEMBL428672 | — | — | 1 | 6.04 |
| CHEMBL1159684 | MENADIONE SULFUROUS ACID | 2.0 | 1 | 4.09 |
| CHEMBL433 | VALPROATE SODIUM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL436 | TOLRESTAT | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL56337 | EPALRESTAT | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL7679 | PONALRESTAT | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL269550 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL266497 | SORBINIL | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL7480 | ALCONIL | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL428672 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1159684 | MENADIONE SULFUROUS ACID | IC50 | = | 82000.0 | nM | 4.09 |
| CHEMBL433 | VALPROATE SODIUM | IC50 | = | 380000.0 | nM | - |